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Antipruritics

a technology of antipruritic and cannabinoid receptor, applied in the field of antipruritic, can solve the problems of not being able to suppress pruritus caused by other diseases, not being able to disclose the effect of agonists and cannabinoid receptors

Inactive Publication Date: 2008-12-18
YASUI KIYOSHI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The compounds with agonistic activity to cannabinoid receptors demonstrate potent antipruritic activity, effectively reducing itching in various disease conditions and preventing associated complications such as scratching-induced disorders.

Problems solved by technology

They are effective against pruritus accompanying with edema and urticaria, but are not enough to suppress pruritus caused by other diseases.
However, these references do not disclose that agonists to the cannabinoid receptor have an antipruritic effect.

Method used

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Examples

Experimental program
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Effect test

example

[0411]For example, a compound having an agonistic activity to the cannabinoid receptor used in the present invention can be prepared as follows.

example a

Preparation of 2-(2-isopropylphenyl)imino-3-(allylthio)thiocarbonyl-5,5-dimethyl-1,3-thiazine (Compound II-1)

[0412]

[0413]To a solution of 2-(2-isopropylphenyl)imino-5,5-dimethyl-1,3-thiazine (0.26 g) obtained by the preparation described in WO 01 / 19087, and carbondisulfide (0.10 g) in N,N-dimethylformamide (3 mL) was added 60% sodium hydride (0.05 g) under ice-cooling. The reaction mixture was stirred for 30 minutes. Allylchloride (0.10 g) was added thereto. The reaction mixture was stirred at 0° C. for 1 h. To the reaction mixture was added water (80 mL), which was extracted with diethylether (100 ml), dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (n-hexane / ethyl acetate) to give 2-(2-isopropylphenyl)imino-3((allylthio)thiocarbonyl-5,5-dimethyl-1,3-thiazine (0.26 g, yield: 69%) as a pale yellow oil.

example b

Preparation of 2-(2-isopropylphenyl)imino-3-(5-trifluoromethyl-2-pyridyl)-5,5-dimethyl-1,3-thiazine (Compound II-106)

[0414]

[0415]To a solution of 2-(2-isopropylphenyl)imino-5,5-dimethyl-1,3-thiazine (0.26 g) obtained by the preparation described in WO 01119087, and 5-trifluoromethyl-2-chloropyridine (0.24 g) in N,N-dimethylformamide (3 mL) was added 60% sodium hydride (0.05 g) under ice-cooling. The mixture was stirred at room temperature for 2 h. To the reaction mixture was added water (80 mL), which was extracted with diethylether (100 mL), dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (n-hexane / ethyl acetate) to give 2-(2-isopropylphenyl)imino-3-(5-trifluoromethyl-2-pyridyl)-5,5-dimethyl-1,3-thiazine (0.13 g, yield: 32%) as colorless oil.

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PUM

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Abstract

It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having an agonistic activity to the cannabinoid receptor shows an antipruritics effect.

Description

TECHNICAL FIELD[0001]The present invention relates to antipruritics, in detail, antipruritics which contains as an active ingredient a compound having an agonistic activity to the cannabinoid receptor.BACKGROUND ART[0002]It is well known that pruritus is produced in diseases such as atopic dermatitis, urticaria, allergic rhinitis and allergic conjunctivitis as well as inflammatory response like edema. Pruritus is the major symptom in allergic skin disorders, for example, atopic dermatitis and urticaria, and is also observed in systemic diseases such as chronic renal failure that requires hemodialysis and cholestatic chronic hepatitis.[0003]At present, antihistamines are used as antipruritics. They are effective against pruritus accompanying with edema and urticaria, but are not enough to suppress pruritus caused by other diseases. Therefore, the development of potent antipruritics (inhibitors for pruritus, stoppers for pruritus, suppressors for pruritus) is expected.[0004]In additio...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4412A61K31/435A61K31/00A61K31/426A61K31/436A61K31/4375A61K31/4439A61K31/4523A61K31/4704A61K31/4709A61K31/4745A61K31/506A61K31/5377A61K31/54A61K31/541A61K31/5415A61K31/547A61P17/04C07D213/69C07D213/70C07D213/75C07D213/82C07D215/38C07D215/54C07D217/26C07D221/04C07D221/12C07D221/22C07D263/46C07D277/18C07D279/06C07D279/08C07D401/04C07D401/06C07D401/12C07D403/06C07D405/12C07D405/14C07D411/12C07D413/12C07D413/14C07D417/04C07D417/06C07D417/12C07D455/06C07D471/04C07D493/04C07D513/04C07D513/10
CPCA61K31/00A61K31/255A61K31/426A61K31/435A61K31/436A61K31/4375A61K31/4412A61K31/4439A61K31/4523A61K31/4704A61K31/4709A61K31/4745A61K31/506A61K31/5377A61K31/54A61K31/541A61K31/5415A61K31/547C07D213/69C07D213/70C07D213/75C07D213/82C07D215/38C07D215/54C07D217/26C07D221/04C07D221/12C07D221/22C07D263/46C07D277/18C07D279/06C07D279/08C07D401/04C07D401/06C07D401/12C07D403/06C07D405/12C07D405/14C07D411/12C07D413/12C07D413/14C07D417/04C07D417/06C07D417/12C07D455/06C07D471/04C07D493/04C07D513/04C07D513/10A61P11/02A61P17/04A61P25/20A61P27/02A61P27/12A61P27/14A61P29/00A61P31/00A61P37/00A61P37/08A61P43/00
Inventor YASUI, KIYOSHIMORIOKA, YASUHIDEHANASAKI, KOHJI
Owner YASUI KIYOSHI
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